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Anti-inflammatory Flavanones and Flavones from Tephrosia linearis.
Journal of Natural Products ( IF 5.1 ) Pub Date : 2020-03-10 , DOI: 10.1021/acs.jnatprod.9b00922
Richard Oriko Owor 1, 2, 3 , Kibrom Gebreheiwot Bedane 2 , Sebastian Zühlke 2 , Solomon Derese 1 , George Otieno Ong'amo 4 , Albert Ndakala 1 , Michael Spiteller 2
Affiliation  

Phytochemical analysis of a methanol-dichloromethane (1:1) extract of the aerial parts of Tephrosialinearis led to the isolation of 18 compounds. Seven of these, namely, lineaflavones A-D (1-4), 6-methoxygeraldone (5), 8″-acetylobovatin (6), and 5-hydroxy-7-methoxysaniculamin A (7) are new compounds. The compounds were characterized based on their NMR and HRMSn data. The anti-inflammatory effects of the crude extract and isolated compounds were evaluated by measuring the levels of interleukins (IL-1β, IL-2, and IL-6), granulocyte-macrophage colony-stimulating factor (GM-CSF), and tumor necrosis factor-α (TNF-α) in lipopolysaccharide (LPS)-stimulated peripheral blood mononuclear cells (PBMCs). The crude extract inhibited the release of all cytokines except IL-1β, which slightly increased in comparison to the LPS control. All the tested compounds suppressed the production of IL-2, GM-CSF, and TNF-α. Whereas compounds 1, 2, 4-8, 10-15, 17, and 18 decreased production of IL-6, compounds 1, 2, 4, 7, 10, 13-15, and 17 inhibited the release of IL-1β. It is worth noting that most of the compounds tested showed a superior reduction in cytokines release compared to the reference drug ibuprofen.

中文翻译:

抗炎黄酮和黄酮类植物。

线虫地上部分的甲醇-二氯甲烷(1:1)提取物的植物化学分析导致​​分离出18种化合物。这些中的七个,即利奈黄酮AD(1-4),6-甲氧基杰拉酮(5),8''-乙酰基卵磷脂(6)和5-羟基-7-甲氧基Saniculamin A(7)是新化合物。根据其NMR和HRMSn数据对化合物进行表征。通过测量白介素(IL-1β,IL-2和IL-6),粒细胞巨噬细胞集落刺激因子(GM-CSF)和肿瘤的水平来评估粗提物和分离的化合物的抗炎作用脂多糖(LPS)刺激的外周血单核细胞(PBMC)中的坏死因子-α(TNF-α)。粗提取物抑制除IL-1β以外的所有细胞因子的释放,与ILS对照相比,IL-1β略有增加。所有测试的化合物均可抑制IL-2,GM-CSF和TNF-α的产生。化合物1、2、4、8、10、15、17和18降低了IL-6的产生,而化合物1,2、4、7、10、13、15和17抑制了IL-1β的释放。值得注意的是,与参考药物布洛芬相比,大多数测试化合物均显示出细胞因子释放的优异降低。
更新日期:2020-03-10
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